大黄酸-N-β-羟乙基替加氟酯的合成及其骨亲和性  

Synthesization of 1,8-dihydroxy-9,10-anthraquinone-2-carboxylic acid-β-(N-tegafur) hydroxy ethyl ester and its bone affinity

作　　者：居晓伟[1] 侯晓华[1] 范桂平[2] 白淑芳[3] 张静泽[3] 安茜[3] 陈虹[3] 

机构地区：[1]武警医学院附属医院药剂科,天津300162 [2]沈阳药科大学,沈阳辽宁110015 [3]武警医学院生药教研室,天津300162

出　　处：《武警医学院学报》2008年第5期375-377,共3页Acta Academiae Medicinae CPAPF

基　　金：国家自然科学基金资助项目(30371682)

摘　　要：【目的】研究大黄酸衍生物的合成方法,探讨其骨亲和性。【方法】将大黄酸与替加氟衍生物耦联合成骨靶向的新型大黄酸衍生物,结构经质谱及核磁共振谱证实。用羟基磷灰石吸附试验评价它的体外骨亲和性。【结果】合成了大黄酸-N-β-羟乙基替加氟酯。实验显示该化合物的骨亲和性与四环素接近。【结论】大黄酸-N-β-羟乙基替加氟酯具有良好的骨亲和性。[Objective] To study the method of synthesizing derivatives of rhein and its bone affinity. [Methods] Rhein was linked to derivative of tegafur to prepare a new derivative of bone-target compound. Its structure was identified by ^1 HNMR and MS. The compound was carried out the bone affinity assay with hydroxyapative adsorption experiment. [Results] 1,8-dihydroxy-9, 10-anthraquinone-2-carboxyhc acid-β- （N-tegafur） hydroxyethyl ester was synthesized. The result shows that the bone affinity of the compound was similer to that of tetracycline. [ Conclusions] 1,8 -dihydroxy-9,10 -anthraquinone-2-carboxylic acid-β- （N-tegafur） hydroxyethyl ester has good bone affinity.

关 键 词：骨靶向 大黄酸衍生物 合成 

分 类 号：R965[医药卫生—药理学]